Antengene Corporation Limited, a leading innovative, global biopharmaceutical company dedicated to discovering, developing and commercializing first-in-class and/or best-in-class medicines for cancer and other life-threatening diseases, announced today that the first patient has been dosed in the Phase Ib/II, open-label multi-center, REACH trial to evaluate ATG-016 (eltanexor) monotherapy in subjects with advanced solid tumors including those with genetic mutations (such as K-ras or p53) or a viral association (such as Epstein Barr Virus (EBV) and Human Papilloma Virus (HPV). Enrollment in the study is already underway.
“The opening of the REACH trial is a very important milestone for Antengene. As the second study of ATG-016 to be conducted in mainland China, it highlights our approach of running our own, complementary, additional studies in China on partnered products,” said Jay Mei, M.D., Ph.D, Founder and CEO of Antengene. “Furthermore, this study underscores Antengene’s commitment to focusing our clinical development efforts on diseases that are particularly prevalent in China versus the US,” continued Dr. Mei.
ATG-016/eltanexor and other SINE (Selective Inhibitor of Nuclear Export) compounds inhibit the nuclear chaperone protein called Exportin 1 (XPO1) that helps cancers grow by removing tumor suppressor proteins from the nucleus. ATG-016 is an orally-active, highly-specific next-generation XPO1 inhibitor with an improved pharmacological profile and reduced brain penetration versus the first novel SINE compound, ATG-010/selinexor. These attributes can potentially enable more frequent dosing and a better tolerated dosing regimen. ATG-016 demonstrated preliminary anti-tumor activity in a Phase I study in advanced solid tumors and hematologic malignancies. SINE compounds also inhibit replication of viruses that utilize XPO1 machinery. In preclinical studies, ATG-016 demonstrated an inhibitory effect on the growth of cancer induced by viruses such as EBV and HPV.
“The REACH study is designed to evaluate the safety, pharmacokinetics and preliminary efficacy of ATG-016/eltanexor monotherapy in patients with progressive or resistant disease, building on promising, published Phase I results. With 70% of cancer patients remaining as non-responders or progressing after initial response, Antengene has prioritized the development of treatments for advanced or resistant cancers,” said Kevin Lynch, M.D., Antengene’s Chief Medical Officer. “We remain grateful to all of the healthcare professionals, scientists, patients, and families involved with Antengene’s clinical studies,” continued Dr. Lynch.
About the REACH Trial
The REACH trial is a multicenter, open-label Phase Ib/II exploratory trial comprising a dose-escalation portion and dose-expansion portion. The initial dose-escalation of ATG-016 will be conducted in patients with advanced solid tumors, to determine the maximum-tolerated dose (MTD), recommended Phase II dose (RP2D), and biologically effective dose of ATG-016. Then the study will proceed to the dose-expansion portion and initiate the Phase II study in patients with relapsed or metastatic penile squamous cell carcinoma or Stage IV nasopharyngeal carcinoma (endemic tumors in China and southeastern in China) to further assess the efficacy and safety of ATG-016 monotherapy. In the Phase II study, investigators will evaluate tumor responses every six weeks using the Response Evaluation Criteria in Solid Tumors Version 1.1 (RECIST1.1).
About the SINE Compounds
SINE (Selective Inhibitor of Nuclear Export) compounds are inhibitors of the major nuclear export protein Exportin 1 (XPO1). Currently, there are three oral SINE compounds, ATG-010 (selinexor), ATG-016 (eltanexor), and ATG-527 (verdinexor), under clinical development. Antengene has an exclusive license from Karyopharm Therapeutics Inc. (“Karyopharm”) to develop and commercialize these compounds in certain APAC markets.
About ATG-010/Selinexor/ XPOVIO®
ATG-010/selinexor (XPOVIO®) is the first-generation SINE compound. Karyopharm developed and secured approval by the US FDA for the treatment of relapsed/refractory multiple myeloma (RRMM) and relapsed, refractory diffuse large B-cell lymphoma.
Antengene secured approval of ATG-010 in South Korea and China through a priority review process. Antengene is conducting 10 additional studies with ATG-010 in mainland China (3 in collaboration with Karyopharm).
About ATG-016/Eltanexor
Karyopharm is conducting a Phase I/II trial for eltanexor in subjects with Myelodysplastic syndrome (MDS).
Antengene is also evaluating ATG-016/eltanexor in the HATCH study, a Phase I/II monotherapy, registration-track study in high-risk MDS patients who have failed hypomethylating agents.
About Antengene
Antengene Corporation Limited (“Antengene”, SEHK: 6996.HK) is a leading clinical-stage R&D- driven global biopharmaceutical company focused on innovative first-in-class/best-in-class therapeutic medicines for cancer and other life-threatening diseases. Driven by its vision of “Treating Patients Beyond Borders”, Antengene aims to provide the most advanced anti-cancer drugs to patients in the Asia Pacific Region and around the world. Since initiating operations in 2017, Antengene has obtained 20 investigational new drug (IND) approvals in the U.S. and in Asia, submitted 6 new drug applications (NDAs) in multiple Asia Pacific markets, with the NDA for selinexor/ATG-010 in South Korea and China approved through a priority review process. Leveraging partnerships as well as in-house drug discovery, Antengene has built a broad and expanding pipeline of 15 clinical and pre-clinical assets. The Company has global rights on 10 programs and Asia Pacific rights, including the Greater China region, on 5 programs.